Studies On Inhibition Of Tumor Proliferation In Vitro Of 10-hydroxycanthin-6-one And Its Ester Derivatives

Natural products are the important source of anti-tumor drugs,at present more than forty percent of clinical medicines are from natural products and their derivatives.Recent pharmacological researches have revealed that the kind of alkaloids possess some anti-tumor activities.According to the existing methods in our laboratory,we synthesized the natural product 10-hydroxycanthin-6-one and 24 ester derivatives.And then the anti-tumor effect of these compounds was analyzed.The results are outlined below:1.The MTT assay was used to study the cytotoxic effect of 10-hydroxycanthin-6-one and its ester derivatives on human tumor cell lines(SGC-7901,A549,He La)and all of them showed cytotoxicity against the tested tumor cells.Besides,the effect on He La cells was stronger than the other two.Here is there probably structure-activity relationship according the inhibition effects: the anti-tumor effects of the aromatic ester derivatives were stronger than the aliphatic ester derivatives.2.According to the MTT results,the compounds F6,F7 m and F7 n were chosen to father find the effects on the apoptosis of He La cells.The three compounds could induce apoptosis measured with Hoechst 33342 stainning and detected by agarose gel electrophoresis.There is also a find that in some degree they could inhibit the migration of the cells through wound experiment.We also found that they caused a increasement in population of cells at G2 stage and a increase in the proportion of apoptosis.We could get a conclusion that was the three compounds induced apoptosis in a dose-dependent manner and they also caused He La cells cycle arrest in the G2 phase.This provides a theoretical basis for developing the anticancer drugs.